PROTACs
PROTAC (PROteolysis-TArgeting Chimera) is a heterobifunctional nanomolecule containing two different ligands, ligand for ubiquitin E3 and ligand for target protein. The two parts are connected by linker to form a "three-unit" polymer, target protein ligand-linker-E3 ligase ligand. Building blocks of PROTAC molecules include PROTAC Linker, Ligand for Target Protein for PROTAC, Ligand for E3 Ligase, E3 Ligase Ligand-Linker Conjugate, Target Protein Ligand-Linker Conjugate, etc.
Alle PROTACs Isoform-spezifische Produkte anzeigen
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PROTACs Verwandte Produkte (1334)
Verwandte Produkte (1334)
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Antibodies (1)
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PROTACs Isoform Comparison
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PROTAC EGFR degrader 16
0 ImagesArt. -Nr.: HY-178242CAS. Nr.: 2654821-07-3PROTAC EGFR degrader 16 (Compound 98) a selective EGFR PROTAC degrader with DC50 values of < 50 nM in NCI-H1975 (EGFR L858R-T970M), NCI-H3225 (EGFR L858R) and NCI-H1976 + CS (EGFR L858R-T970M-L797S). PROTAC EGFR degrader 16 can be used for the study of EGFR-driven cancerssuch as non-small cell lung cancer (Pink: EGFR ligand (HY-178313); Blue: CRBN ligand (HY-W1128702); Black: Linker; EGFR ligand + Linker (HY-178311)).
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BWA-6047
0 ImagesArt. -Nr.: HY-176128BWA-6047 is an oral active PROTAC degrader targeting AR/AR-V7 and GSPT1 with DC50 values of 3.7, 3.0 and 1.2 nM in 22Rv1 cells. BWA-6047 suppresses the expression of AR downstream target genes and and transcriptional activity. BWA-6047 inhibits cancer cells proliferation, causes G1 phase cell cycle arrest and induces apoptosis. BWA-6047 increases cleaved-PARP-1 and cleaved-caspase-3 levels. BWA-6047 reduces growth of LNCaP xenograft tumors in mice models without obvious toxicity. BWA-6047 can be used for the research of prostate cancer.
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PROTAC SARS-CoV-2 Mpro degrader-1
0 ImagesArt. -Nr.: HY-157804CAS. Nr.: 3029579-46-9PROTAC SARS-CoV-2 Mpro degrader-1 is a SARS-CoV-2 Mpro PROTAC degrader with a DC50 of 18.1 μM. PROTAC SARS-CoV-2 Mpro degrader-1 recruits the Von-Hippel Lindau (VHL) E3 ligase to mediate ubiquitination and proteasomal degradation of SARS-CoV-2 Mpro, without inhibiting the catalytic activity of Mpro. PROTAC SARS-CoV-2 Mpro degrader-1 exhibits broad-spectrum antiviral activity against coronaviruses (SARS-CoV-2, HCoV-OC43, HCoV-229E). PROTAC SARS-CoV-2 Mpro degrader-1 can be used in studies related to SARS-CoV-2 infection, HCoV-OC43 infection, and HCoV-229E infection.
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CST905
0 ImagesArt. -Nr.: HY-175435CAS. Nr.: 3094183-98-6
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PROTAC Axl Degrader 1
0 ImagesArt. -Nr.: HY-144624CAS. Nr.: 3033401-47-4PROTAC Axl Degrader 1 is an orally active PROTAC degrader targeting the AXL receptor tyrosine kinase, with an IC50 of 0.92 μM against human targets. PROTAC Axl Degrader 1 induces cytoplasmic vacuolization, methuosis (macropinocytosis-induced cell death), excessive macropinosome production, and Rac1 activation. PROTAC Axl Degrader 1 inhibits the proliferation and migration of cancer cells. PROTAC Axl Degrader 1 can be used in breast cancer-related research.
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GNE-5472
0 ImagesArt. -Nr.: HY-175445CAS. Nr.: 2417369-99-2GNE-5472 is a potent bifunctional ERα PRRTAC degrader, with its E3 ligand being a pan-IAP antagonist. GNE-5472 antagonizes cIAP1/2, activating the non-classical NF-κB pathway, resulting in a significant upregulation of TNFα expression. GNE-5472 inhibits the proliferation of breast cancer cells and induces cell apoptosis. GNE-5472 can be used for the study of breast cancer.
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PROTAC EZH2 Degrader-9
0 ImagesArt. -Nr.: HY-179499CAS. Nr.: 2978620-84-5PROTAC EZH2 Degrader-9 is orally active EZH2 PROTAC degrader degrading EZH2 via the ubiquitin-proteasome pathway. PROTAC EZH2 Degrader-9 downregulates PRC2 core subunits and potent inhibition of H3K27me3 without affecting common CRBN neosubstrates while it was selective over GSp'T1 and ikZF1/3. PROTAC EZH2 Degrader-9 exhibits potent antiproliferative activity against multiple cancer cell lines by inducing cell cycle and apoptosis. PROTAC EZH2 Degrader-9 reverses PRC2-mediated gene silencing and inhibiting EZH2 non-catalytic target gene activation. PROTAC EZH2 Degrader-9 can be used for leukemia, lymphoma, and non-small cell lung cancer research.
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CXJ2080
0 ImagesArt. -Nr.: HY-183070CXJ2080 is a selective PROTAC-based CDK7 degrader with a DC50 of 0.88 nM. CXJ2080 recruits VHL E3 ligase to induce ubiquitin-proteasome-dependent CDK7 degradation, disrupts the CDK7-cyclin H-MAT1 complex, suppresses CDK7-dependent phosphorylation of RNA polymerase II CTD Ser5, CDK1 Thr161, and CDK2 Thr160. CXJ2080 activates the p53-p21 axis, suppresses MYC-driven signaling, induces leukemia cell cycle arrest, apoptosis, and differentiation, reduces CD117 expression, spares platelets and normal PBMCs, maintains sustained CDK7 degradation post-washout. CXJ2080 can be used for the research of acute leukemia.
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PROTAC BTK Degrader-5
0 ImagesArt. -Nr.: HY-155072CAS. Nr.: 3049086-75-8PROTAC BTK degraders-5(compound 3e) is a selective BTK PROTAC degrader with a DC50 value of 7.0 nM in JeKo-1 cells. PROTAC BTK degraders-5 has no off-target effect on degrading CRBN neosubstates. PROTAC BTK degraders-5 has anti-proliferation effect on various lymphoma tumor cells and can be used in chronic lymphoid malignancies research.
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PROTAC AR Degrader-11
0 ImagesArt. -Nr.: HY-177694CAS. Nr.: 2798907-41-0PROTAC AR Degrader-11 is a potent androgen receptor and androgen receptor splice variant-7 PROTAC degrader. PROTAC AR Degrader-11 shows potent cytotoxicity against both CWR22RV1 cells and VCaP cells. PROTAC AR Degrader-11 can be used in prostate cancer research.
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PROTAC EZH2 Degrader-26
0 ImagesArt. -Nr.: HY-181327CAS. Nr.: 2641601-66-1
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CH091138
0 ImagesArt. -Nr.: HY-175025CH091138 is a potent and selective KRASG12D PROTAC degrader with DC50s of 148.3 nM in HeLa cells and 469.8 nM in AsPC-1 cells. CH091138 selectively degrades exogenous and endogenous KRASG12D but not KRASWT or other KRAS mutants (G12C/G12S/G12V), depending on the VHL-mediated ubiquitin-proteasome system. CH091138 exhibits potent anti-tumor activity and induces cancer cell apoptosis. CH091138 can be used for the studies of pancreatic cancer and colon cancer. (Pink: KRASG12D ligand (HY-175144); Blue: VHL E3 ligase ligand (HY-138678); Black: Linker; VHL E3 ligase ligand + Linker (HY-136006B)).
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SJ44236
0 ImagesArt. -Nr.: HY-170900SJ44236 is a BET PROTAC degrader with activity against BRD2, BRD3 and BRD4 (DC50 = 127 pM). SJ44236 induces ubiquitination and proteasomal degradation by forming a ternary complex with BET proteins and CRBN-DDB1. SJ44236 downregulates c-Myc, upregulates p53 and reduces cancer cell viability. SJ44236 can be used for the research of leukemia and medulloblastoma.
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PROTAC hCAII degrader-1
0 ImagesArt. -Nr.: HY-179467CAS. Nr.: 2892306-56-6PROTAC hCAII degrader-1 is a potent PROTAC human carbonic anhydrase II (hCAII) degrader with an DC50 of 0.5 nM in HEK293 cells. PROTAC hCAII degrader-1 recruits cereblon (CRBN) E3 ubiquitin ligase to form a ternary complex. PROTAC hCAII degrader-1 enables ubiquitination and subsequent proteasomal degradation of hCAII.
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PROTAC NAMPT Degrader-1
0 ImagesArt. -Nr.: HY-163440CAS. Nr.: 3102963-15-2
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EBET-1593
0 ImagesArt. -Nr.: HY-177244CAS. Nr.: 3031540-97-0EBET-1593 is a BET PROTAC degrader. EBET-1593 can promote the ubiquitination and degradation of BET. EBET-1593 is a lead payload. EBET-1593 can be used to synthesize ADCs, such as 84-EBET. 84-EBET has antitumor effects against pancreatic ductal adenocarcinoma.
